Molecular Weight(MW): 541.02
Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
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G, tumor growth response of HR6 tumors grown in athymic nude mice and treated with single and combination treatments. H, table of earliest detectable (P < 0.05) reduction in tumor size for control versus treated mice. ^, tumors that initially shrank and then grew; NS, not significant. I, OMI index initially decreases in HR6 organoids treated with paclitaxel, XL147, and combination therapies at 24 hours. J, OMI index of HR6 organoids treated for 72 hours. Red bars, significant reductions in OMI index; P< 0.05, for treated organoids versus control. Blue bars, significant increases in OMIindex;P< 0.05, for treated organoids versus control.
Cancer Res, 2014, 74(18):5184-5194.. Pilaralisib (XL147) purchased from Selleck.
Purity & Quality Control
Choose Selective PI3K Inhibitors
|Description||Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.|
Pilaralisib exhibits cytotoxic activity in Pediatric Preclinical Testing Program (PPTP) cell lines, with a median relative IC50 value of 10.9 mM (range 2.7 mM to 24.5 mM).
|In vivo||In BALB/c nu/nu mice, Pilaralisib (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts. Pilaralisib is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals. In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.|
|Kinase Assay: ||
In vitro kinase inhibition assays:Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively
-  Foster P, et al. Mol Cancer Ther. 2015, 14(4), 931-940.
-  Reynolds CP, et al. Pediatr Blood Cancer. 2013, 60(5), 791-798.
-  Chakrabarty A, et al. Proc Natl Acad Sci U S A. 2012, 109(8), 2718-2723.
|In vitro||DMSO||100 mg/mL warmed (184.83 mM)|
|In vivo||Add solvents individually and in order:
10 mM HCl in sterile water
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01357330||Completed||Solid Tumors||Sanofi||May 2011||Phase 1|
|NCT01240460||Completed||Glioblastoma|Astrocytoma, Grade IV||Sanofi||January 2011||Phase 1|
|NCT01082068||Completed||Breast Cancer||Sanofi||June 2010||Phase 1|Phase 2|
|NCT01042925||Completed||Breast Cancer|Breast Neoplasms||Sanofi||February 2010||Phase 1|Phase 2|
|NCT01013324||Completed||Endometrial Cancer|Endometrial Neoplasms||Sanofi||January 2010||Phase 2|
|NCT00756847||Completed||Cancer|Non-Small Cell Lung Cancer|Endometrial Carcinoma|Ovarian Carcinoma||Sanofi||September 2008||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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